Background:

SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities[1][2].

SZL P1-41 (5-20μM; 24 hours) induces endogenous p27 protein expression in PC3 cells and also induced expression of p21, another Skp2 substrate[1].

SZL P1-41 (40-80 mg/kg; i.p.) displays a potent effect on inhibiting prostate and lung tumor growth in Nude mice bearing A549 and PC3 tumor xenografts[1].

参考文献:
[1]. Chan CH et al. Pharmacological inactivation of Skp2 SCF ubiquitin ligase restricts cancer stem cell traits and cancer progression. Cell. 2013 Aug 1;154(3):556-68.
[2]. Chan CH, et al. Skp2: a dream target in the coming age of cancer therapy. Cell Cycle. 2014;13(5):679-80.